Dimeric 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HM...

created [InstanceEdit:9705585] Jassal, Bijay, 2020-10-27
dbId 9705590
displayName Dimeric 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HM...
modified [InstanceEdit:9969889] D'Eustachio, Peter, 2025-10-23
schemaClass Summation
text Dimeric 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMGCR dimer) is the key enzyme in the cholesterol biosynthetic pathway and catalyzes the committed step of the reduction of beta-hydroxy-3-methylglutaryl CoA (bHMG-CoA) to mevalonate. HMGCR is regarded as one of the most important drug targets in the treatment of hypercholesterolemia. HMGCR inhibitors, commonly referred to as statins, are among the most widely prescribed drugs in the world. Statins work by their similarity to the substrate (bHMG-CoA), leading to competition towards the HMG binding site on the enzyme between substrate and statins (Istvan & Deisenhofer 2001). As statins also block the access of the substrate to the binding site, the affinity of HMGCR for statins is slightly higher than its affinity for the substrate (Istvan 2002, Carbonell & Ernesto Freire 2005, Gesto et al. 2020). Statins can be divided in two types, according to their origin. Type I statins e.g. lovastatin, pravastatin and simvastatin, are natural fungal products and Type II statins e.g. atorvastatin, rosuvastatin and fluvastatin, are fully synthetic.
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